Assay Detail
Functional
CHEMBL841894
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Inhibition of electrically evoked twitches of isolated guinea pig ileal segments induced by methyl-histamine in the absence and presence of antagonist.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 21 | 7.44 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL114085 | — | — | 1 | 8.60 |
| CHEMBL321835 | — | — | 1 | 8.40 |
| CHEMBL322481 | — | — | 1 | 8.30 |
| CHEMBL326624 | — | — | 1 | 8.30 |
| CHEMBL420124 | — | — | 1 | 8.20 |
| CHEMBL326081 | — | — | 1 | 8.00 |
| CHEMBL112629 | — | — | 1 | 8.00 |
| CHEMBL112670 | — | — | 1 | 7.90 |
| CHEMBL112301 | — | — | 1 | 7.90 |
| CHEMBL113181 | — | — | 1 | 7.70 |
| CHEMBL116270 | — | — | 1 | 7.60 |
| CHEMBL115091 | — | — | 1 | 7.50 |
| CHEMBL325645 | — | — | 1 | 7.30 |
| CHEMBL112753 | — | — | 1 | 7.20 |
| CHEMBL112676 | — | — | 1 | 7.00 |
| CHEMBL324724 | — | — | 1 | 6.80 |
| CHEMBL112202 | — | — | 1 | 6.70 |
| CHEMBL115169 | — | — | 1 | 6.60 |
| CHEMBL113404 | — | — | 1 | 6.20 |
| CHEMBL113403 | — | — | 1 | 6.20 |
| CHEMBL112099 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL114085 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL321835 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL322481 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL326624 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL420124 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL326081 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL112629 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL112670 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL112301 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL113181 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL116270 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL115091 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL325645 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL112753 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL112676 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL324724 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL112202 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL115169 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL113404 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL113403 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL112099 | — | Kd | = | 1584.89 | nM | 5.80 |